Use my Search Websuite to scan PubMed, PMCentral, Journal Hosts and Journal Archives, FullText.
Kick-your-searchterm to multiple Engines kick-your-query now !>
A dictionary by aggregated review articles of nephrology, medicine and the life sciences
Your one-stop-run pathway from word to the immediate pdf of peer-reviewed on-topic knowledge.

suck abstract from ncbi


suck pdf from google scholar
unlimited free pdf from europmc23788528    free
PDF from PMC    free
html from PMC    free
PDF vom PMID23788528  :  Publisher

suck abstract from ncbi

Nephropedia Template TP Text

Twit Text FOAVip

Twit Text #

English Wikipedia

  • Synergistic inhibitor binding to the papain-like protease of human SARS coronavirus: mechanistic and inhibitor design implications #MMPMID23788528
  • Lee H; Cao S; Hevener KE; Truong L; Gatuz JL; Patel K; Ghosh AK; Johnson ME
  • ChemMedChem 2013[Aug]; 8 (8): 1361-72 PMID23788528show ga
  • We previously developed two potent chemical classes that inhibit the essential papain-like protease (PLpro) of severe acute respiratory syndrome coronavirus. In this study, we applied a novel approach to identify small fragments that act synergistically with these inhibitors. A fragment library was screened in combination with four previously developed lead inhibitors by fluorescence-based enzymatic assays. Several fragment compounds synergistically enhanced the inhibitory activity of the lead inhibitors by approximately an order of magnitude. Surface plasmon resonance measurements showed that three fragments bind specifically to the PLpro enzyme. Mode of inhibition, computational solvent mapping, and molecular docking studies suggest that these fragments bind adjacent to the binding site of the lead inhibitors and further stabilize the inhibitor-bound state. We propose potential next-generation compounds based on a computational fragment-merging approach. This approach provides an alternative strategy for lead optimization for cases in which direct co-crystallization is difficult.
  • |*Drug Design[MESH]
  • |Antiviral Agents/*chemistry/metabolism[MESH]
  • |Binding Sites[MESH]
  • |Coronavirus 3C Proteases[MESH]
  • |Cysteine Endopeptidases/metabolism[MESH]
  • |Drug Synergism[MESH]
  • |Humans[MESH]
  • |Kinetics[MESH]
  • |Molecular Docking Simulation[MESH]
  • |Protease Inhibitors/*chemistry/metabolism[MESH]
  • |Protein Binding[MESH]
  • |Protein Structure, Tertiary[MESH]
  • |SARS Virus/*enzymology[MESH]
  • |Small Molecule Libraries/chemistry/metabolism[MESH]
  • |Surface Plasmon Resonance[MESH]
  • |Viral Proteins/*antagonists & inhibitors/metabolism[MESH]

  • DeepDyve
  • Pubget Overpricing
  • suck abstract from ncbi

    1361 8.8 2013